E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo
E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo
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DOI：
10.1016/s0959-8049(01)00275-1
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发表时间：
2001-11-01
影响因子：
8.4
通讯作者：
Yoshimatsu, K
中科院分区：
文献类型：
--
作者：
Ozawa, Y;Sugi, NH;Yoshimatsu, K
E7070(N-(3-Chloro-7-indolyl)-1，4-benzenedisulphonamide)是通过抗肿瘤筛选和流式细胞仪分析从我们的磺胺类化合物中挑选出来的。经E7070处理后，P388小鼠白血病细胞周期进程受阻于G1期。对人结肠癌HCT116细胞的杀伤作用呈时间依赖性。在42个人类肿瘤细胞系的研究小组中，E7070显示出一种与临床上使用的其他抗癌药物不同的抗癌光谱。使用人类肿瘤异种移植模型进行的动物实验表明，E7070不仅可以抑制肿瘤的生长，而且可以导致五分之三的结直肠癌和两例肺癌的肿瘤消退。在HCT116异种移植模型中，E7070优于5-FU、MMC和CPT-11(伊立替康)。此外，在接受E7070治疗的小鼠中，80%的晚期LVI肿瘤完全消退。所有这些观察都促进了该药物的临床评价。(C)2001爱思唯尔科学有限公司。保留所有权利。
E7070 (N-(3-Chloro-7-indolyl)-1,4-benzenedisulphonamide) was selected from our sulphonamide compound collections via antitumour screening and flow cytometric analysis. Following treatment with E7070, the cell cycle progression of P388 murine leukaemia cells was disturbed in the G I phase. The cell-killing effect on human colon cancer HCT116 cells was found to be time-dependent. In the panel of 42 human tumour cell lines, E7070 showed an antitumour spectrum that was distinct from those of other anticancer drugs used in clinic. Animal tests using human tumour xenograft models demonstrated that E7070 could cause not only tumour growth suppression, but also tumour regression in three of five colorectal and two of two lung cancers. In the HCT116 xenograft model, E7070 was shown to be superior to 5-FU, MMC and CPT-11 (irinotecan). Furthermore, complete regression of advanced LVI tumours was observed in 80% of E7070-treated mice. All of these observations have promoted this drug to clinical evaluation. (C) 2001 Elsevier Science Ltd. All rights reserved.